| 货号 | 11593-1mg |
| 描述 | Three related forms of the kinase Akt (1, 2, 3, also known as protein kinase B isoforms PKBα, β, γ) modulate cell proliferation, metabolism, and survival as well as angiogenesis.1,2 MK-2206 is an orally active, allosteric Akt inhibitor that is equally potent toward purified human recombinant Akt1 and Akt2 (IC50s = 5 and 12 nM, respectively) and approximately 5-fold less potent against human Akt3 (IC50 = 65 nM).3 In combination with other anticancer agents including topoisomerase inhibitors, antimetabolites, antimicrotubule agents, DNA cross-linkers or growth factor inhibitors, MK-2206 has been shown to synergistically inhibit cell proliferation of human cancer cell lines.3 At 5 μM, MK-2206 significantly enhances apoptosis in hematopoietic cells treated with chemotherapeutics.4 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Manning, B.D. and Cantley, L.C. AKT/PKB signaling: Navigating downstream. Cell 129, 1261-1274 (2007). 2.Yuan, T.L. and Cantley, L.C. PI3K pathway alterations in cancer: Variations on a theme. Oncogene 27(41), 5497-5510 (2008). 3.Hirai, H.,Sootome, H.,Nakatsuru, Y., et al. MK-2206, an allosteric Akt inhibitor, enhances antitumor efficacy by standard chemotherapeutic agents or molecular targeted drugs in vitro and in vivo. Molecular Cancer Therapeutics 9(7), 1956-1967 (2010). 4.Kurosu, T.,Nagao, T.,Wu, N., et al. Inhibition of the PI3K/Akt/GSK3 pathway downstream of BCR/ABL, Jak2-V617F, or FLT3-ITD downregulates DNA damage-induced Chk1 activation as well as G2/M arrest and prominently enhances induction of apoptosis. PLoS One 8(11), (2013). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 480.4 |
| 分子式 | C25H21N5O • 2HCl |
| CAS号 | 1032350-13-2 |
| 稳定性 | ≥ 2 years |
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